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Enzomenib

Chemical Structure : Enzomenib

CAS No.: 2412555-70-3

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Enzomenib (DSP-5336, DSP5336)

Catalog No.: PC-22768Not For Human Use, Lab Use Only.

Enzomenib (DSP-5336) is a potent, and orally bioavailable menin-MLL interaction inhibitor with IC50 of 1.4 nM, directly binds to the menin protein with Kd of 6 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    Enzomenib (DSP-5336) is a potent, and orally bioavailable menin-MLL interaction inhibitor with IC50 of 1.4 nM, directly binds to the menin protein with Kd of 6 nM.
    DSP-5336 selectively inhibited the cell growth of human leukemia cell lines including MV-4-11, MOLM-13, KOPN-8, and OCI-AML3 (IC 50 = 10, 15, 31 and 15 nM, respectively).
    DSP-5336 did not affect the cell growth of human leukemia cell lines such as HL-60, MOLT-4, and Reh (IC50>10 uM), which do not have MLL-r or NPM1 mutations.
    DSP-5336 exhibited a signicant antitumor activity at the doses of 25 mg/kg and 50 mg/kg, administered twice daily (BID) for 20 days, mouse xenograft model using MV-4-11 cells, which express MLL-AF4.

    Physicochemical Properties

    M.Wt 419.41
    Formula C20H20F3N5O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    Benzamide, 5-fluoro-2-[[4-[7-[[(1S,3S,4R)-5-methylene-2-azabicyclo[2.2.2]oct-3-yl]carbonyl]-2,7-diazaspiro[3.5]non-2-yl]-5-pyrimidinyl]oxy]-N,N-bis(1-methylethyl)-

    References

    1. Ken Eguchi, et al. Blood, Volume 138, Supplement 1, 23 November 2021, Page 3339

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